Recent interest in the possible existence of a close relationship between the action of glyoxalase and the regulation of cellular growth has prompted us to establish a program to study the glyoxalase system with respect to the preparation and enzymatic evaluation of selective reversible and irreversible inhibitors of this system. These compounds will have the potential as possible anticancer agents by interfering selectively with a biochemical system which may play a role in regulation of cell division. Many ketoaldehydes have been shown to possess carcinostatic and antiviral activity. Since these compounds are rapidly metabolized by glyoxalase, the inhibition of this enzyme becomes a vital target in enhancing the activity of the ketoaldehydes.